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European Journal of Drug Metabolism and Pharmacokinetics

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https://www.readbyqxmd.com/read/28929443/short-term-fasting-alters-pharmacokinetics-of-cytochrome-p450-probe-drugs-does-protein-binding-play-a-role
#1
Laureen A Lammers, Roos Achterbergh, Johannes A Romijn, Ron A A Mathôt
BACKGROUND AND OBJECTIVES: Short-term fasting differentially alters cytochrome P450 (CYP) mediated drug metabolism. This has been established by using CYP-enzyme selective probe drugs. However, the observed effects of fasting on the pharmacokinetics of these probe drugs may also include the effects of altered plasma protein binding of these drugs. Therefore, we studied the effect of short-term fasting on protein binding of five commonly used probe drugs [caffeine (CYP1A2), metoprolol (CYP2D6), midazolam (CYP3A4), omeprazole (CYP2C19) and S-warfarin (CYP2C9)]...
September 19, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28916980/pharmacokinetics-of-panax-notoginseng-saponins-in-adhesive-and-normal-preparation-of-fufang-danshen
#2
Xiao-Nan Chen, Dan-Qi Li, Meng-di Zhao, Gang-Yan Yu, Shou-Ying Du, Yang Lu, Jie Bai, Peng-Yue Li, Ya-Li Wu, Zhi-Hao Tian, Yan-Ying Zeng
BACKGROUND AND OBJECTIVE: Fufang Danshen formula, a famous Chinese patent medicine containing Salvia miltiorrhiza, Panax notoginseng and borneol, has been widely used in the treatment of coronary heart disease. The application is restricted by low bioavailability partly due to Panax notoginseng saponins (PNS) instability and low in vivo absorption. Thus, adhesive pellets were developed to improve bioavailability. The objectives of the present study were to evaluate the adhesive preparation by describing PNS's plasma pharmacokinetics in vivo and compare adhesive micro pills with normal preparation...
September 15, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28916907/pharmacokinetic-study-of-piracetam-in-focal-cerebral-ischemic-rats
#3
Pankaj Paliwal, Debabrata Dash, Sairam Krishnamurthy
BACKGROUND AND OBJECTIVE: Cerebral ischemia affects hepatic enzymes and brain permeability extensively. Piracetam was investigated up to phase III of clinical trials and there is lack of data on brain penetration in cerebral ischemic condition. Thus, knowledge of the pharmacokinetics and brain penetration of piracetam during ischemic condition would aid to improve pharmacotherapeutics in ischemic stroke. METHODS: Focal cerebral ischemia was induced by middle cerebral artery occlusion for 2 h in male Wistar rats followed by reperfusion...
September 15, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28913815/pharmacokinetic-pharmacodynamic-analysis-of-cisplatin-with-hydration-and-mannitol-diuresis-the-contribution-of-urine-cisplatin-concentration-to-nephrotoxicity
#4
Keizo Fukushima, Akira Okada, Hiroyuki Oe, Mika Hirasaki, Mami Hamori, Asako Nishimura, Nobuhito Shibata, Nobuyuki Sugioka
BACKGROUND AND OBJECTIVES: Forced diuresis, high-volume hydration with diuresis, is widely used as a prophylactic treatment against cisplatin nephrotoxicity. However, the details of the underlying mechanisms and the optimal protocol of forced diuresis remain unclear. The present study investigated the alterations in pharmacokinetics and pharmacodynamics (nephrotoxicity) of cisplatin with forced diuresis treatment. METHODS: Cisplatin (5 mg/kg) was intravenously injected to rats (5 rats/group, except for control group in pharmacodynamic study, n = 13) treated with or without forced diuresis 2-h pre- and post-hydration with 10% mannitol at different infusion rates (0...
September 14, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28895074/in-vitro-comparison-of-the-role-of-p-glycoprotein-and-breast-cancer-resistance-protein-on-direct-oral-anticoagulants-disposition
#5
Sophie Hodin, Thierry Basset, Elodie Jacqueroux, Olivier Delezay, Anthony Clotagatide, Nathalie Perek, Patrick Mismetti, Xavier Delavenne
BACKGROUND: Pharmacokinetics of direct oral anticoagulants (DOACs) are influenced by ATP-binding cassette (ABC) transporters such as P-glycoprotein (P-gp) and Breast Cancer Resistance Protein (BCRP). OBJECTIVES: To better understand the role of transporters in DOAC disposition, we evaluated and compared the permeabilities and transport properties of these drugs. METHODS: Bidirectional permeabilities of DOACs were investigated across Caco-2 cells monolayer...
September 11, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28890991/comments-on-population-pharmacokinetic-modeling-of-olmesartan-the-active-metabolite-of-olmesartan-medoxomil-in-patients-with-hypertension
#6
LETTER
Nuggehally R Srinivas
No abstract text is available yet for this article.
September 11, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28801891/monitoring-of-busulphan-concentrations-in-children-undergone-hematopoietic-stem-cell-transplantation-unicentric-experience-over-10%C3%A2-years
#7
Maura Faraci, Carmine Tinelli, Edoardo Lanino, Stefano Giardino, Massimiliano Leoni, Marta Ferretti, Elio Castagnola, Monica Broglia, Annalisa De Silvestri, Daniela Di Martino, Antonella Bartoli
BACKGROUND AND OBJECTIVES: The aim of this report is to describe the experience in the management of busulphan-based conditioning regimen administered before hematopoietic stem cell transplantation (HSCT) in children. METHODS: We report the values of the first dose AUC (area under the concentration-time curve, normal target between 3600 and 4800 ng·h/mL) in children treated with oral and intravenous busulphan, and we analyze the impact of some clinical variables in this cohort of patients...
August 11, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28795390/potential-influence-of-endothelial-adsorption-on-the-delayed-time-to-maximum-concentration-of-biopharmaceuticals
#8
Joannes A A Reijers, Martijn J C Dane, Anton Jan van Zonneveld, Jacobus Burggraaf, Matthijs Moerland
BACKGROUND AND OBJECTIVES: Maximum plasma concentration of biopharmaceuticals sometimes occurs long after completion of intravenous infusion. The objective of this research was to study the hypothetical adsorption of biopharmaceuticals to endothelium and infusion material, which may theoretically explain this phenomenon. METHODS: Infusion procedures were mimicked in an artificial vessel covered with a confluent monolayer of endothelial cells. Three monoclonal antibodies (MAbs) and C1 inhibitor were studied...
August 9, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28702877/absorption-distribution-metabolism-and-excretion-of-14-c-volixibat-in-healthy-men-phase-1-open-label-study
#9
Nicholas Siebers, Melissa Palmer, Debra G Silberg, Lee Jennings, Caleb Bliss, Patrick T Martin
BACKGROUND AND OBJECTIVES: Volixibat is a potent inhibitor of the apical sodium-dependent bile acid transporter in development for the treatment of nonalcoholic steatohepatitis. This phase 1, open-label study investigated the absorption, distribution, metabolism, and excretion of [(14)C]-volixibat in heathy men. METHODS: Eligible men (n = 8) aged 18-50 years (body mass index 18.0-30.0 kg/m(2); weight >50 kg) received a single oral dose of [(14)C]-volixibat 50 mg containing ~5...
July 12, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28688001/pharmacokinetic-interactions-and-safety-of-coadministration-of-glecaprevir-and-pibrentasvir-in-healthy-volunteers
#10
Chih-Wei Lin, Sandeep Dutta, Weihan Zhao, Armen Asatryan, Andrew Campbell, Wei Liu
BACKGROUND AND OBJECTIVE: Glecaprevir and pibrentasvir are pangenotypic direct-acting antiviral agents for the treatment of chronic hepatitis C virus infection. The aim of the present study was to evaluate the drug-drug interaction and safety of glecaprevir and pibrentasvir coadministration in healthy volunteers. METHODS: In this open-label, randomized, multiple-dose, Phase 1 study in 72 subjects, glecaprevir (100-1200 mg once daily) and pibrentasvir (40-200 mg once daily) were administered alone for 7 days and then in combination for another 7 days...
July 7, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28688000/is-rpmi-2650-a-suitable-in-vitro-nasal-model-for-drug-transport-studies
#11
REVIEW
Clément Mercier, Nathalie Perek, Xavier Delavenne
The evaluation of new intranasal medications requires the development of in vitro cell model suitable for high-throughput screening studies. The aim of a pharmacological model is to closely mimic the barrier properties of human nasal mucosa that will influence drug pharmacokinetics. In this context, the human nasal cell line RPMI 2650 has been investigated over these last years. Although the initial studies tended to demonstrate strong physiological correlations between RPMI 2650 cells and nasal mucosa, the variability of experimental designs does not allow a clear comparison of actual data...
July 7, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28685495/effects-of-metformin-and-furosemide-on-rosuvastatin-pharmacokinetics-in-healthy-volunteers-implications-for-their-use-as-probe-drugs-in-a-transporter-cocktail
#12
Peter Stopfer, Thomas Giessmann, Kathrin Hohl, Ashish Sharma, Naoki Ishiguro, Mitchell E Taub, Arvid Jungnik, Dietmar Gansser, Thomas Ebner, Fabian Müller
BACKGROUND: In a recently described probe drug cocktail for clinically relevant drug transporters containing digoxin, furosemide, metformin and rosuvastatin, mutual interactions were essentially absent except for increases in the systemic exposure of rosuvastatin. To optimize the cocktail, we further examined the dose dependence of the effects of metformin and furosemide on rosuvastatin pharmacokinetics. METHODS: This was a randomized, open label, single center, six-treatment, six-period, six-sequence crossover trial...
July 6, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28064418/novel-antiretroviral-drugs-in-patients-with-renal-impairment-clinical-and-pharmacokinetic-considerations
#13
Dario Cattaneo, Cristina Gervasoni
Highly active antiretroviral therapy (HAART) has dramatically increased the survival of HIV-infected patients from Western countries reducing the incidence of opportunistic infections and AIDS-related malignancies, and improving the patients' quality of life compared with the pre-HAART era. HIV is thus now considered in the West as a chronic disease, with the majority of HIV-infected patients successfully reaching an optimal immune and virological outcome a few months after starting HAART. However, this switch from acute to chronic disease has been accompanied by an increased incidence of chronic kidney disease (CKD), reported in up to 60% of HIV-infected patients...
August 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27928655/in-vivo-pharmacokinetics-of-puerarin-via-different-drug-administration-routes-based-on-middle-cerebral-artery-occlusion-model
#14
Pengyue Li, Jie Bai, Boyu Dong, Yang Lu, Shengwei Zhang, Shuang Guo, Ning Tan, Mengdi Zhao, Shouying Du, Puning Cao
BACKGROUND AND OBJECTIVES: Pueraria labata has traditionally been applied in the treatment of stroke in Chinese clinics. Puerarin is the key ingredient in it for brain protection effect. To find a superior administration route for puerarin in the treatment of ischemic cerebrovascular disease, the pharmacokinetics of puerarin based on the middle cerebral artery occlusion (MCAO) rat via different administration routes were studied and compared. METHODS: Ten rats (MCAO model) divided into two groups were treated with puerarin via intravenous and intranasal routes...
August 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27889876/population-pharmacokinetic-pharmacodynamic-modeling-of-5-fluorouracil-for-toxicities-in-rats
#15
Shinji Kobuchi, Yukako Ito, Toshiyuki Sakaeda
BACKGROUND AND OBJECTIVES: Myelosuppression is a dose-limiting toxicity of 5-fluorouracil (5-FU). Predicting the inter- and intra-patient variability in pharmacokinetics and toxicities of 5-FU may contribute to the individualized medicine. This study aimed to establish a population pharmacokinetic-pharmacodynamic model that could evaluate the inter- and intra-individual variability in the plasma 5-FU concentration, 5-FU-induced body weight loss and myelosuppression in rats. METHOD: Plasma 5-FU concentrations, body weight loss, and blood cell counts in rats following the intravenous administration of various doses of 5-FU for 4 days were used to develop the population pharmacokinetic-pharmacodynamic model...
August 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27864798/pharmacokinetic-drug-interactions-with-panax-ginseng
#16
REVIEW
Meenakshi R Ramanathan, Scott R Penzak
Panax ginseng is widely used as an adaptogen throughout the world. The major active constituents of P. ginseng are ginsenosides. Most naturally occurring ginsenosides are deglycosylated by colonic bacteria to intestinal metabolites. Ginsenosides along with these metabolites are widely accepted as being responsible for the pharmacologic activity and drug interaction potential of ginseng. Numerous preclinical studies have assessed the influence of various ginseng components on cytochrome P450 (CYP), glucuronidation, and drug transport activity...
August 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27858342/physiologically-based-pharmacokinetic-pbpk-modeling-of-pitavastatin-and-atorvastatin-to-predict-drug-drug-interactions-ddis
#17
Peng Duan, Ping Zhao, Lei Zhang
BACKGROUND: The disposition of statins varies and involves both metabolizing enzymes and transporters, making predictions of statin drug-drug interactions (DDIs) challenging. Physiologically based pharmacokinetic (PBPK) models have, however, demonstrated ability to predict complex DDIs. OBJECTIVE: In this study, PBPK models of two statins (pitavastatin and atorvastatin) were developed and applied to predict pitavastatin and atorvastatin associated DDIs. METHOD: Pitavastatin and atorvastatin PBPK models were developed using in vitro and human pharmacokinetic data in a population-based PBPK software (SimCYP(®)) by considering the contribution of both metabolizing enzymes and transporters to their overall pharmacokinetics...
August 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27853934/evaluation-of-in-vitro-cytochrome-p450-inhibition-and-in-vitro-fate-of-structurally-diverse-n-oxide-metabolites-case-studies-with-clozapine-levofloxacin-roflumilast-voriconazole-and-zopiclone
#18
Poonam Giri, Sneha Naidu, Nirmal Patel, Harilal Patel, Nuggehally R Srinivas
BACKGROUND AND OBJECTIVES: The role of metabolite(s) to elicit potential clinical drug-drug interaction (DDI) via cytochrome P450 enzymes (CYP) is gaining momentum. In this context, the role of N-oxides for in vitro CYP inhibition has not been evaluated. The objectives of this study were: (a) to examine in vitro CYP inhibition of N-oxides of clozapine, levofloxacin, roflumilast, voriconazole and zopiclone in a tiered approach and (b) evaluate in vitro fate of aforementioned N-oxides examined in recombinant CYPs, human microsomes and hepatocytes...
August 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27815731/hepatic-uptake-mechanism-of-ophiopogonin-d-mediated-by-organic-anion-transporting-polypeptides
#19
Wen Zhang, Xiaomin Xiong, Lin Chen, Mingyi Liu, Yuqing Xiong, Hong Zhang, Shibo Huang, Chunhua Xia
BACKGROUND AND OBJECTIVES: Ophiopogonin D (OPD) is one of the main active ingredients of SMI (Shenmai injection) which is widely used in clinical practice in China. Our previous study indicated  that OPD might be transported from blood into liver mediated by organic anion transporting polypeptides (OATPs/oatps). This study aims to explore the hepatic uptake mechanism of OPD in rat and human. METHODS: Rosuvastatin (a competitive inhibitor of oatp1b2, oatp1a1, and oatp1a4), glycyrrhizic acid (a specific inhibitor of oatp1b2), digoxin (a specific inhibitor of oatp1a4), bromosulfophthalein (BSP), and ibuprofen (a specific inhibitor of oatp1a1) were used to study the uptake of OPD in rat hepatocytes...
August 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27778300/liver-perfusion-modifies-gd-dtpa-and-gd-bopta-hepatocyte-concentrations-through-transfer-clearances-across-sinusoidal-membranes
#20
Jean-Luc Daire, Benjamin Leporq, Valérie Vilgrain, Bernard E Van Beers, Sabine Schmidt, Catherine M Pastor
BACKGROUND AND OBJECTIVES: Gadobenate dimeglumine (Gd-BOPTA) is a commercialised hepatobiliary contrast agent used during liver magnetic resonance imaging (MRI) to detect liver diseases. It enters into human hepatocytes through organic anion transporting polypeptides (OATP1B1/B3) and crosses the canalicular transporter multiple resistance-associated protein 2 (MRP2) to be excreted into bile canaliculi. Gd-BOPTA can return to sinusoids via the sinusoidal transporters MRP3/MRP4. Hepatocyte concentrations of Gd-BOPTA depend on three clearances: the sinusoidal clearance or volume of sinusoidal blood cleared of drugs per unit of time and two hepatocyte clearances (into bile canaliculi or back to sinusoids) or volume of hepatocytes cleared of drugs per unit of time in the respective liver compartments...
August 2017: European Journal of Drug Metabolism and Pharmacokinetics
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